The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis of the target compounds was accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug selectively into the cancer cells to be hydrolyzed by enzymes that are elevated in tumor tissues compared with normal tissues . Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.
Abstract
The study aims to clarify the impact of the adoption of the International Financial Reporting Standard (IFRS16) on lease contracts in the General Iraqi Insurance Company on the financial statements, and thus the impact on financial ratios and indicators, Since the financial reporting standard considers lease contracts as an asset called the right to use the asset and is offset by a liability, this changes the way the financial statements are presented, with an addition to both the asset and liability sides. In order to show the extent to which the adoption of the standard reflects on the financial performance
... Show MoreBackground: diabetic mellitus is one of the serious systemic diseases that may cause general systemic changes, which may be reflected in the oral cavity. The aims of this study were to assess the severity of dental caries, Mutans Streptococci and Lactobacilli in addition to flow rate and pH among uncontrolled and controlled diabetic groups in comparison with non-diabetic control group. Materials and Methods: Study groups consisted of 25 uncontrolled diabetic patients (HbA1c > 7), 25 controlled diabetic patients (HbA1c ? 7), in addition to 25 non-diabetic healthy looking individuals. Their age was (18-22) years from both genders. The diagnosis and recording of dental caries was according to severity of dental caries lesion through the applic
... Show MoreThe influence of 5-10 kHz audio frequency on the power dissipation in ac discharge of argon gas was studied experimentally, at pressures 50-80 mTorr and electrodes separation 10 cm (pd range 0.5-0.8 Torr.
cm). The measurements have shown that the discharge behavior in the ac circuit is equivalent to a series RC circuit. It is observed that the variation curve of discharge power P with the frequency f is approximately has a Gaussian shape. It is also observed that the curve of Pm- pd is the inverse of Paschen curve, where Pm is the maximum power in the frequency range. The time of breakdown is estimated from the curve of P- f.
Abstract
The aim of the study is to study the relationship between strategic orientation and organizational performance. The strategic direction is the main purpose for which the organization is found. Therefore, it is the main engine for all the activities and tasks that the institution can carry out to achieve its objectives within the environment in which it operates. ,. The research problem was formed by several questions to determine the level of the strategic direction and the nature of its relationship with organizational performance in the Iraqi Ministry of Defense / Inspector General's Office as the field of application to answer. The sample was selected by a sample of 60 individuals, department managers, And the que
Lead toxicity elicits neurological damage which is a well-known disorder that has been considered to be a major cause for multiple condition such as behavioral defect; mental retardation; and nerve insufficient activity.
This research is designed to estimate potential protective effect of vinpocetine on neurotoxicity stimulated by lead acetate in rats.
Eighteen adult rats of both sexes were randomly enrolled into three groups. Each group includes 6 rats as followings: Group I- Rats were given 0.3ml normal saline solution orally; then intraperitoneal injection of 100μl of the normal saline was given 1h later; this group was considered as control. Group II- Rats were given an intraperitoneal injection of 20mg/kg lead acetate
... Show MoreBackground: Any child with Down's syndrome does not develop in the same manner as normal child. Therefore, the child should not be viewed as being like everyone else. Developmental enamel defects in primary teeth have been found at least twice as frequently in disabled children as in control children. Down's syndrome consumed protein more than the recommended daily allowance compared to other disabled groups. Therefore, the aim of this study was to investigate developmental defects of enamel and their relations to nutrient intake among Down's syndrome children in comparison to normal children. Materials and Methods: A sample consisted of fifty institutionalized Down's syndrome children (study group) and 50 normal children (control group)
... Show MoreBackground: Change in palatal vault shape and Reinforcement of high impact acrylic denture base resin may in turn affect the dimensional accuracy of acrylic resin and affecting the fitness of the denture.This study evaluated tostudy the effect of fiber reinforcement for high-impact acrylic resin denture base with different palatal vault shapes on adaptation or gap space between the denture base and the stone cast and compare with non-fiber reinforcement and effect of palatal vault shapes on adaptation of non-reinforced and fiber reinforced high impact denture base acrylic resin Material and method: Three different palatal vault shapes were prepared on standard casts using CNC (computer numerical control) machine. 60 samples of heat polymeri
... Show MoreBackground: Polymethylmethacrylate (PMMA) has relatively unsatisfactory mechanical properties such as low flexural strength and impact strength also dimensional instability. Material and method: Zirconium silicate nanoparticles were coated with a layer of trimethoxysilylpropylmethacrylate (TMSPM) before sonication in monomer (MMA) with the percentages 1% and 1.5% by weight then mixed with powder using conventional procedure, (150) samples were prepared and divided into three groups, each group consisted of (50) samples, the first group prepared from PMMA without addition (control), another group with the addition of 1% wt Zrsio4 nanoparticles (experimental) and the third one with 1.5% wt Zrsio4 nanoparticles (experimental). Each group
... Show More